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1. 发明授权

US4758584A Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
标题翻译：由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4758584A
公开(公告)日：1988-07-19
申请号：US011183
申请日：1987-02-05
申请人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
发明人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
IPC分类号： C07D233/54 , C07D401/12 , C07D417/12 , C07K5/02 , A61K37/64 , C07K5/08
CPC分类号： C07D233/64 , C07D401/12 , C07D417/12 , C07K5/0227 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译：式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，亚磺酰基或磺酰基，R 6代表取代的氨基，具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

2. 发明授权

US4914129A Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
标题翻译：由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4914129A
公开(公告)日：1990-04-03
申请号：US405372
申请日：1989-09-08
申请人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
发明人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
IPC分类号： C07D233/54 , C07D233/64 , C07D233/84 , C07D401/12 , C07D417/12
CPC分类号： C07D233/64 , C07D233/84 , C07D401/12 , C07D417/12 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

3. 发明授权

US4727060A Novel 5-amino-4-hydroxyvaleryl derivatives 失效
标题翻译：新型5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4727060A
公开(公告)日：1988-02-23
申请号：US794914
申请日：1985-11-04
申请人： Peter Buhlmayer , Vittorio Rasetti , Walter Fuhrer , James L. Stanton , Richard Goschke
发明人： Peter Buhlmayer , Vittorio Rasetti , Walter Fuhrer , James L. Stanton , Richard Goschke
IPC分类号： A61K38/00 , C07C53/136 , C07C57/58 , C07C59/48 , C07C59/68 , C07C59/84 , C07D209/16 , C07D209/42 , C07D209/52 , C07D215/48 , C07D233/54 , C07D233/64 , C07D263/04 , C07D263/06 , C07D295/13 , C07D307/81 , C07D401/12 , C07D403/12 , C07D405/12 , C07F7/18 , C07K5/02 , C07K5/078 , A61K37/43 , C07K5/08 , C07K5/06
CPC分类号： C07D233/64 , C07C53/136 , C07C57/58 , C07C59/48 , C07C59/68 , C07C59/84 , C07D209/16 , C07D209/42 , C07D209/52 , C07D215/48 , C07D263/04 , C07D263/06 , C07D295/13 , C07D307/81 , C07D401/12 , C07D403/12 , C07D405/12 , C07F7/1852 , C07F7/1856 , C07K5/0207 , C07K5/06139 , A61K38/00 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, A represents an optionally N-alkylated .alpha.-amino acid residue which is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl having 2 or more carbon atoms, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy or optionally substituted mercapto and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as antihypertensives.
摘要翻译：式（I）的化合物，其中R 1表示氢或酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R 1和C-末端键合在基团-NR 2 - ，R 2上代表氢或低级烷基，R3代表氢，低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表具有2个或更多碳原子的低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基或任选取代的巯基，R 6表示取代的氨基，以及具有成盐基团的化合物的盐抑制酶肾素的增压作用，可用作抗高血压药。

4. 发明授权

US4889869A Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
标题翻译：由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4889869A
公开(公告)日：1989-12-26
申请号：US341239
申请日：1989-04-19
申请人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
发明人： Peter Buhlmayer , James L. Stanton , Walter Fuhrer , Richard Goschke , Vittorio Rasetti , Heinrich Rueger
IPC分类号： C07D233/54 , C07D233/64 , C07D233/84 , C07D401/12 , C07D417/12
CPC分类号： C07D233/64 , C07D233/84 , C07D401/12 , C07D417/12 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulyhinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译：式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，磺酰基或磺酰基，R 6代表取代的氨基，具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

5. 发明授权

US4931591A Novel 5-amino-4-hydroxyvaleryl derivatives 失效
标题翻译：新型5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4931591A
公开(公告)日：1990-06-05
申请号：US380711
申请日：1989-07-12
申请人： Peter Buhlmayer , Vittorio Rasetti , Walter Fuhrer , James L. Stanton , Richard Goschl
发明人： Peter Buhlmayer , Vittorio Rasetti , Walter Fuhrer , James L. Stanton , Richard Goschl
IPC分类号： A61K38/00 , C07C53/136 , C07C57/58 , C07C59/48 , C07C59/68 , C07C59/84 , C07D209/16 , C07D209/42 , C07D209/52 , C07D215/48 , C07D233/54 , C07D233/64 , C07D263/04 , C07D263/06 , C07D295/13 , C07D307/81 , C07D401/12 , C07D403/12 , C07D405/12 , C07F7/18 , C07K5/02 , C07K5/078
CPC分类号： C07D233/64 , C07C53/136 , C07C57/58 , C07C59/48 , C07C59/68 , C07C59/84 , C07D209/16 , C07D209/42 , C07D209/52 , C07D215/48 , C07D263/04 , C07D263/06 , C07D295/13 , C07D307/81 , C07D401/12 , C07D403/12 , C07D405/12 , C07F7/1852 , C07F7/1856 , C07K5/0207 , C07K5/06139 , A61K38/00 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, A represents an optionally N-alkylated .alpha.-amino acid residue which is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl having 2 or more carbon atoms, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy or optionally substituted mercapto and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as antihypertensives.

6. 发明授权

US4863903A Substituted 5-amino-4-hydroxyvaleryl derivatives 失效
标题翻译：取代的5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4863903A
公开(公告)日：1989-09-05
申请号：US112631
申请日：1987-10-26
申请人： Walter Fuhrer , Peter Buhlmayer , Vittorio Rasetti , Bernhard Riniker
发明人： Walter Fuhrer , Peter Buhlmayer , Vittorio Rasetti , Bernhard Riniker
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D213/40 , C07D233/54 , C07D277/46 , C07D295/13 , C07F7/18 , C07K1/113 , C07K5/02 , C07K9/00
CPC分类号： C07D213/40 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D233/64 , C07D277/46 , C07D295/13 , C07F7/1852 , C07K5/0207 , C07K5/0227 , C07K9/001 , A61K38/00 , Y10S530/80 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group -NR.sub.2 -, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl-lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译：式（I）的化合物，其中R 1表示氢或酰基，X 1表示任选N-烷基化的氨基酸残基，其N-末端与R 1和C-末端键合于X 2，X 2表示任选N-烷基化的氨基酸残基，其N-末端与X1和C-末端键合在基团-NR2-上，R 2表示氢或低级烷基，R 3表示氢，烷基，环烷基，芳基 - 低级烷基或芳基，R 4表示羟基或醚化或酯化羟基，R5代表烷基，环烷基，芳基 - 低级烷基或芳基，R6表示游离或取代的氨基或取代的羟基，这些具有成盐基团的化合物的盐抑制酶肾素的增压作用，用作抗高血压药。

7. 发明授权

US4613676A Substituted 5-amino-4-hydroxyvaleryl derivatives 失效
标题翻译：取代的5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4613676A
公开(公告)日：1986-09-23
申请号：US671261
申请日：1984-11-14
申请人： Walter Fuhrer , Peter Buhlmayer , Vittorio Rasetti , Bernhard Riniker
发明人： Walter Fuhrer , Peter Buhlmayer , Vittorio Rasetti , Bernhard Riniker
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D213/40 , C07D233/54 , C07D277/46 , C07D295/13 , C07F7/18 , C07K1/113 , C07K5/02 , C07K9/00 , C07C101/30 , C07C69/74 , C07C101/72 , C07C61/08
CPC分类号： C07D213/40 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D233/64 , C07D277/46 , C07D295/13 , C07F7/1852 , C07K5/0207 , C07K5/0227 , C07K9/001 , A61K38/00 , Y10S530/80 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl- lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译：式（I）的化合物，其中R 1表示氢或酰基，X 1表示任选N-烷基化的氨基酸残基，其N-末端与R 1和C-末端键合于X 2，X 2表示任选N-烷基化的氨基酸残基，其N-末端与X1和C-末端键合在基团-NR2-上，R 2表示氢或低级烷基，R 3表示氢，烷基，环烷基，芳基 - 低级烷基或芳基，R 4表示羟基或醚化或酯化羟基，R5代表烷基，环烷基，芳基 - 低级烷基或芳基，R6表示游离或取代的氨基或取代的羟基，这些具有成盐基团的化合物的盐抑制酶肾素的增压作用，用作抗高血压药。

8. 发明授权

US4719288A Substituted 5-amino-4-hydroxyvaleryl derivatives 失效
标题翻译：取代的5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4719288A
公开(公告)日：1988-01-12
申请号：US869800
申请日：1986-06-02
申请人： Walter Fuhrer , Peter Buhlmayer , Vittorio Rasetti , Bernhard Riniker
发明人： Walter Fuhrer , Peter Buhlmayer , Vittorio Rasetti , Bernhard Riniker
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D213/40 , C07D233/54 , C07D277/46 , C07D295/13 , C07F7/18 , C07K1/113 , C07K5/02 , C07K9/00 , C07K5/08 , C07C103/34 , C07C103/12 , C07C103/20 , C07C101/30 , C07D277/20 , C07D209/18 , C07D233/64 , C07D207/12 , C07D211/70
CPC分类号： C07D213/40 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/42 , C07C255/43 , C07C255/44 , C07D209/16 , C07D233/64 , C07D277/46 , C07D295/13 , C07F7/1852 , C07K5/0207 , C07K5/0227 , C07K9/001 , A61K38/00 , Y10S530/80 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl-lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.
摘要翻译：式（I）的化合物，其中R 1表示氢或酰基，X 1表示任选N-烷基化的氨基酸残基，其N-末端与R 1和C-末端键合于X 2，X 2表示任选N-烷基化的氨基酸残基，其N-末端与X1和C-末端键合在基团-NR2-上，R 2表示氢或低级烷基，R 3表示氢，烷基，环烷基，芳基 - 低级烷基或芳基，R 4表示羟基或醚化或酯化羟基，R5代表烷基，环烷基，芳基 - 低级烷基或芳基，R6表示游离或取代的氨基或取代的羟基，这些具有成盐基团的化合物的盐抑制酶肾素的增压作用，用作抗高血压药。

9. 发明申请

US20090131437A1 DISUBSTITUTED UREAS AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的消除性尿路炎
公开(公告)号：US20090131437A1
公开(公告)日：2009-05-21
申请号：US11813067
申请日：2006-01-03
申请人： Pascal Furet , Georg Martiny-Baron , Clive McCarthy , Vittorio Rasetti , Andrea Vaupel
发明人： Pascal Furet , Georg Martiny-Baron , Clive McCarthy , Vittorio Rasetti , Andrea Vaupel
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14
摘要： The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.
摘要翻译：本发明涉及式（I）化合物，其作为激酶抑制剂的用途，包含所述化合物的新药物制剂，用于诊断或治疗温血动物，特别是人的所述化合物，其用于治疗疾病或用于制造可用于治疗对激酶活性调节作出反应的疾病的药物制剂，包括将所述化合物施用于温血动物，特别是人的治疗方法，以及所述化合物的制备方法。

10. 发明授权

US5719141A 2,9-diamino- and 2-amino-8-carbamoyl-4-hydroxy-alkanoic acid amide derivatives 失效
标题翻译： 2,9-二氨基 - 和2-氨基-8-氨基甲酰基-4-羟基 - 链烷酰胺衍生物
公开(公告)号：US5719141A
公开(公告)日：1998-02-17
申请号：US525254
申请日：1995-09-08
申请人： Vittorio Rasetti , Heinrich Rueger , Jurgen Klaus Maibaum , Robert Mah , Markus Grutter , Nissim Claude Cohen
发明人： Vittorio Rasetti , Heinrich Rueger , Jurgen Klaus Maibaum , Robert Mah , Markus Grutter , Nissim Claude Cohen
IPC分类号： A61K31/16 , A61K31/165 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/5355 , A61K31/538 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61P9/12 , C07C237/04 , C07C237/06 , C07C237/22 , C07C271/20 , C07C271/22 , C07D207/00 , C07D209/00 , C07D209/08 , C07D209/42 , C07D211/00 , C07D211/34 , C07D211/60 , C07D213/40 , C07D213/75 , C07D213/89 , C07D215/00 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/36 , C07D215/38 , C07D215/54 , C07D215/56 , C07D217/02 , C07D221/12 , C07D223/16 , C07D235/04 , C07D235/06 , C07D235/08 , C07D239/70 , C07D239/74 , C07D241/00 , C07D241/36 , C07D241/44 , C07D265/28 , C07D265/34 , C07D265/36 , C07D279/12 , C07D279/14 , C07D279/16 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/12 , C07D411/02 , C07D413/02
CPC分类号： C07D213/40 , C07C237/06 , C07C237/22 , C07C271/20 , C07D209/08 , C07D209/42 , C07D211/34 , C07D213/89 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/36 , C07D215/38 , C07D215/54 , C07D215/56 , C07D217/02 , C07D221/12 , C07D223/16 , C07D235/06 , C07D239/74 , C07D241/44 , C07D265/36 , C07D279/16 , C07D401/04 , C07D401/12 , C07D413/04
摘要： Compounds of the formula I ##STR1## in which R.sub.1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R.sub.2 and R.sub.3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R.sub.4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R.sub.5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R.sub.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R.sub.7 is hydrogen or lower alkyl, or R.sub.6 and R.sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R.sub.8 denotes an aliphatic, cycloaliphatic-aliphatic or heteroarylaliphatic radical, and their salts can be used as active ingredients for medicaments for treatment of high blood pressure.
摘要翻译：其中R 1是芳基氨基，N-芳基-N-（低级烷氧基 - 低级烷基） - 氨基，N-芳基-N-芳基 - 低级烷基 - 氨基或杂环基的式I化合物（I）环碳原子，X是羰基或亚甲基，R2和R3彼此独立地是氢或低级烷基，或者与它们所键合的碳原子一起是亚环烷基，R4是氢，低级烷基，低级烷酰基或低级烷氧基羰基，R5是羟基，低级烷酰氧基或低级烷氧基羰基氧基，R6是氢，低级烷基，低级烯基，低级炔基，环烷基，环烷基 - 低级烷基，具有5-7个环原子的芳基 - 低级烷基或杂芳基 - 低级烷基在杂芳基环中，R 7为氢或低级烷基，或者R 6和R 7与它们所键合的碳原子一起为环亚烷基，R 8表示脂族，脂环族 - 脂族或杂芳基脂肪族基团，它们的盐可以是用作治疗药物的有效成分 t的高血压。

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